WO2023278300A1 - Forme posologique solide de n-1-pyrrolidine-n-5-(3-trifluorométhoxy)phényl biguanide et ses utilisations - Google Patents

Forme posologique solide de n-1-pyrrolidine-n-5-(3-trifluorométhoxy)phényl biguanide et ses utilisations Download PDF

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Publication number
WO2023278300A1
WO2023278300A1 PCT/US2022/035084 US2022035084W WO2023278300A1 WO 2023278300 A1 WO2023278300 A1 WO 2023278300A1 US 2022035084 W US2022035084 W US 2022035084W WO 2023278300 A1 WO2023278300 A1 WO 2023278300A1
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WO
WIPO (PCT)
Prior art keywords
hours
cancer
dosage form
solid dosage
administration
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Application number
PCT/US2022/035084
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English (en)
Other versions
WO2023278300A8 (fr
Inventor
Dean WELSCH
Thomas E. Richardson
Original Assignee
ImmunoMet Therapeutics, Inc.
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Publication date
Application filed by ImmunoMet Therapeutics, Inc. filed Critical ImmunoMet Therapeutics, Inc.
Publication of WO2023278300A1 publication Critical patent/WO2023278300A1/fr
Publication of WO2023278300A8 publication Critical patent/WO2023278300A8/fr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material

Abstract

L'invention concerne des formes posologiques solides de N-1-pyrrolidine-N-5-(3-trifluorométhoxy)phényl biguanide, ou un sel pharmaceutiquement acceptable de celui-ci, la forme posologique solide comprenant un revêtement entérique, et leurs utilisations.
PCT/US2022/035084 2021-06-28 2022-06-27 Forme posologique solide de n-1-pyrrolidine-n-5-(3-trifluorométhoxy)phényl biguanide et ses utilisations WO2023278300A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202163215706P 2021-06-28 2021-06-28
US63/215,706 2021-06-28
US202263268103P 2022-02-16 2022-02-16
US63/268,103 2022-02-16

Publications (2)

Publication Number Publication Date
WO2023278300A1 true WO2023278300A1 (fr) 2023-01-05
WO2023278300A8 WO2023278300A8 (fr) 2023-02-09

Family

ID=84691523

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2022/035084 WO2023278300A1 (fr) 2021-06-28 2022-06-27 Forme posologique solide de n-1-pyrrolidine-n-5-(3-trifluorométhoxy)phényl biguanide et ses utilisations

Country Status (2)

Country Link
US (1) US20230000820A1 (fr)
WO (1) WO2023278300A1 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130177604A1 (en) * 2012-01-06 2013-07-11 Elcelyx Therapeutics, Inc. Compositions and Methods of Treating Metabolic Disorders
US20140127299A1 (en) * 2012-11-07 2014-05-08 NaZura BioHealth, Inc. GRAS Enteric Coating Formulations and Methods of Making and Using Same
US9539238B2 (en) * 2015-05-13 2017-01-10 Immunomet Therapeutics, Inc Pharmaceutical composition comprising a biguanide derivative as an active ingredient for preventing or treating glioblastoma
US9540325B2 (en) * 2011-08-08 2017-01-10 ImmunoMet Therapeutics, Inc. N1-cyclic amine-N5-substituted phenyl biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same
US20200093750A1 (en) * 2013-01-05 2020-03-26 Alain D. Baron Compositions and methods for treating metabolic disorders

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6451808B1 (en) * 2000-10-17 2002-09-17 Depomed, Inc. Inhibition of emetic effect of metformin with 5-HT3 receptor antagonists

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9540325B2 (en) * 2011-08-08 2017-01-10 ImmunoMet Therapeutics, Inc. N1-cyclic amine-N5-substituted phenyl biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same
US20130177604A1 (en) * 2012-01-06 2013-07-11 Elcelyx Therapeutics, Inc. Compositions and Methods of Treating Metabolic Disorders
US20140127299A1 (en) * 2012-11-07 2014-05-08 NaZura BioHealth, Inc. GRAS Enteric Coating Formulations and Methods of Making and Using Same
US20200093750A1 (en) * 2013-01-05 2020-03-26 Alain D. Baron Compositions and methods for treating metabolic disorders
US9539238B2 (en) * 2015-05-13 2017-01-10 Immunomet Therapeutics, Inc Pharmaceutical composition comprising a biguanide derivative as an active ingredient for preventing or treating glioblastoma

Also Published As

Publication number Publication date
US20230000820A1 (en) 2023-01-05
WO2023278300A8 (fr) 2023-02-09

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